An overview on performance and image enhancing drugs (PIEDs) confiscated in Italy in the period 2017-2019.

CONTEXT: The illegal market of counterfeit and falsified medicines and supplements containing unlabeled pharmaceuticals is expanding worldwide. They are usually referred to by the term "performance and image enhancing drugs" (PIEDs) and are mainly steroids, stimulants, hormones, and drugs for erectile dysfunction. PIEDs are easily accessible through the online or black markets. We analyzed over 400 such medicines confiscated in Italy in the period 2017-2019, to determine their composition. METHODS: Confiscated products were analyzed by gas chromatography/mass spectrometry and liquid chromatography/high-resolution mass spectrometry, in order to ascertain their composition and to evaluate the correspondence between what was declared on the label and the actual content, or to identify unknown products. RESULTS: The most commonly found substance was anabolic steroids, found in 64% of products, with 11% containing hormone modulators, 6% stimulants, 6% sexual enhancers (mainly sildenafil) and other drugs, including thyroid hormones, melanin stimulators, and vitamins. These substances were often in mixtures. The products were often mislabeled, containing contaminants in addition to the drug declared, or consisted of a drug completely different from the one reported on the label. Fifteen percent of products had a qualitative composition completely different from that declared, while 10% of products showed cross-contamination with other drugs, mainly testosterone esters, probably due to the presence of residues of other drugs in the production line. In addition, 11% of products were not labeled, so their purported composition was unknown. DISCUSSION: PIEDs pose a threat to public health. The main risks are related to the intrinsic toxicity of the substances found, especially when taken without a therapeutic indication. Another issue is related to the mislabeling of the fake medicines, and the poor-quality standard of counterfeit product preparation, with additional risks of the presence of other toxic ingredients or microbial contamination. CONCLUSIONS: The use of counterfeit products is a public health concern, as it constitutes a high risk for consumer health. It is mainly caused by the uncontrolled use of steroids, stimulants, sexual enhancers, and other medicaments, without medical indication or supervision, with variable and unknown compositions and doses, as well as other contaminants as a result of the absence of good manufacturing practices.

Caffeine and Doping-What Have We Learned since 2004.

Caffeine is a naturally occurring plant alkaloid and is found in plant constituents such as coffee and cocoa beans, tea leaves, guarana berries and the kola nut [...].

Potential Risk of Higenamine Misuse in Sports: Evaluation of Lotus Plumule Extract Products and a Human Study.

Since 2017, higenamine has been added to the World Anti-Doping Agency (WADA) prohibited list as a ß2-agonist prohibited at all times for sportspersons. According to WADA's report, positive cases of higenamine misuse have been increasing yearly. However, higenamine occurs naturally in the Chinese herb lotus plumule-the green embryo of lotus (Nelumbo nucifera Gaertn) seeds-commercially available as concentrated powder on the Asian market. This study evaluated the major phytochemical components of lotus plumule products using an appropriate extraction method, followed by a human study in which the products were orally administered in multiple doses to investigate the risk of doping violations. Comparing various extraction methods revealed that optimized microwave-assisted extraction exhibited the highest extraction efficiency (extraction time, 26 min; power, 1046 W; and temperature, 120 °C). Subsequently, the alkaloids in lotus plumule products were quantitatively confirmed and compared. Human study participants (n = 6) consumed 0.8 g of lotus plumule (equivalent to 679.6 µg of higenamine) three times daily for three consecutive days. All participants' urinary higenamine concentrations exceeded the WADA reporting cut-off of 10.0 ng/mL. Accordingly, lotus plumule consumption may engender adverse analytical findings regarding higenamine. Athletes should avoid consuming lotus plumule-containing products during in- and out-of-competition periods.

Liquid chromatography-quadrupole time of flight mass spectrometric method for targeted analysis of 111 nitrogen-based compounds in weight loss and ergogenic supplements.

The use of supplements for weight loss and in sports as pre-workout (ergogenic) products is widespread. Many of these supplements were found to contain active components, which were not claimed on the products labels. A validated liquid chromatography high-resolution mass spectrometry quadrupole time-of-flight (LC-QToF-MS) method was developed for the simultaneous analysis of 111 amine-based compounds belonging to ergogenics, anorectics and other active components including phenethylamines (amphetamines, ephedrines), sibutramine or yohimbine. This method involves the detection of [M+H]+ ions and the separation was achieved using a C18 column, water/acetonitrile gradient as the mobile phase. The method was validated for linearity, repeatability, accuracy, stability, system suitability, limits of quantification (LOQ) and limits of detection (LOD). The limits of detection were in the range from 0.001-0.5 µg/mL. The validated method was applied to the analysis of twenty-seven weight loss and ergogenic dietary supplements. Two-thirds of the supplements contained compounds that were not listed on the product's label. These include several phenethylamines (PEA) such as demelverine, hordenine, N, N-dimethyl-phenethylamine, synephrine, N-methyl-ß-phenethylamine, and methylsynephrine. In addition, the PEA mimics such as dimethylamylamine, dimethylbutylamine other stimulants including fursultiamine, evodiamine, phenibut and theophylline were also observed. One or more of the ingredients listed on the labels were not detected in forty-four percent of the products analyzed. Positive identification was based on retention time, accurate mass and fragment ions in comparison with the respective reference standards. Development of such methods is anticipated to be of aid to regulatory agencies for the identification of undeclared exogenous components that are found in many dietary supplement products.

Severe and protracted cholestasis in 44 young men taking bodybuilding supplements: assessment of genetic, clinical and chemical risk factors.

BACKGROUND: Bodybuilding supplements can cause a profound cholestatic syndrome. AIM: To describe the drug-Induced liver injury network's experience with liver injury due to bodybuilding supplements. METHODS: Liver injury pattern, severity and outcomes, potential genetic associations, and exposure to anabolic steroids by product analysis were analysed in prospectively enrolled subjects with bodybuilding supplement-induced liver injury with causality scores of probable or higher. RESULTS: Forty-four males (mean age 33 years) developed liver injury with a median latency of 73 days. Forty-one per cent presented with hepatocellular pattern of liver injury as defined by the R > 5 ([Fold elevation of ALT] ÷ [Fold elevation of Alk Phos] (mean, range = 6.4, 0.5-31.4, n = 42) despite all presenting with clinical features of cholestatic liver injury (100% with jaundice and 84% with pruritus). Liver biopsy (59% of subjects) demonstrated a mild hepatitis and profound cholestasis in most without bile duct injury, loss or fibrosis. Seventy-one per cent were hospitalised, and none died or required liver transplantation. In some, chemical analysis revealed anabolic steroid controlled substances not listed on the label. No enrichment of genetic variants associated with cholestatic syndromes was found, although mutations in ABCB11 (present in up to 20%) were significantly different than in ethnically matched controls. CONCLUSIONS: Patients with bodybuilding supplements liver injury uniformly presented with cholestatic injury, which slowly resolved. The ingested products often contained anabolic steroids not identified on the label, and no enrichment in genetic variants was found, indicating a need for additional studies.

Common Ingredient Profiles of Multi-Ingredient Pre-Workout Supplements.

Multi-ingredient pre-workout supplements are a popular class of dietary supplements which are purported to improve exercise performance. However, the composition of these products varies substantially between formulations, thus making comparisons challenging. Therefore, the purpose of this study was to identify a common ingredient profile of top-selling pre-workout supplements and to compare ingredient dosages to established efficacious values. The top 100 commercially available pre-workout products were analyzed for listed ingredients and amounts, if available, from the supplement facts panel. The mean ± SD number of ingredients per supplement (n = 100) was 18.4 ± 9.7 with 8.1 ± 9.9 of these ingredients included in a proprietary blend at undisclosed quantities. Relative prevalence and average amounts of the top ingredients amounted to: Beta-alanine (87%; 2.0 ± 0.8 g), Caffeine (86%; 254.0 ± 79.5 mg), Citrulline (71%; 4.0 ± 2.5 g), Tyrosine (63%; 348.0 ± 305.7 mg), Taurine (51%; 1.3 ± 0.6 g), and Creatine (49%; 2.1 ± 1.0 g). Nearly half (44.3%) of all ingredients were included as part of a proprietary blend with undisclosed amounts of each ingredient. The average amount of beta-alanine per serving size was below the recommended efficacious dose. The average caffeine content was near the low end for an effective relative dose for a 70 kg individual (3⁻6 mg·kg-1 of bodyweight).

What's in Your Beet Juice? Nitrate and Nitrite Content of Beet Juice Products Marketed to Athletes.

Consumption of beetroot juice (BRJ) supplements has become popular among athletes, because beets tend to be rich in nitrate (NO3-), which can enhance exercise performance by increasing nitric oxide production. The NO3- content of beets can vary significantly, however, making it difficult to know how much NO3- any product actually contains. Samples from 45 different lots of 24 different BRJ products from 21 different companies were therefore analyzed for NO3- (and nitrite; NO2-) concentration using high performance liquid chromatography. The NO3- and NO2- content, i.e., amount per serving, was then calculated based on either 1) the manufacturer's recommended serving size (for prepackaged/single dose products) or 2) as used in previous studies, a volume of 500 mL (for BRJ sold in bulk containers). There was moderate-to-large variability in NO3- content between samples of the same product, with a mean coefficient of variation of 30±26% (range 2 to 83%). There was even greater variability between products, with a ~50-fold range in NO3- content between the lowest and highest. Only five products consistently provided ≥5 mmol of NO3- per serving, which seems to be the minimal dose required to enhance exercise performance in most individuals. NO2- contents were generally low (i.e., ≤0.5% compared to NO3-), although two products contained 10 and 14%. The present results may be useful to athletes and their support staff contemplating which (if any) BRJ product to utilize. These data may also offer insight into variability in the literature with respect to the effects of BRJ on exercise performance.

A probable case of doping in an Olympic athlete coming back from ancient Greece (V cent. B.C.).

We present here the hypothesis of doping in an athlete coming back from the ancient Greece, dating back to V century B.C. There are some bone alterations due to the sports that he probably practiced, and that are represented on the amphorae (prices of his victories) found near his sepulchre. The skeleton shows a considerable mass and bone density. The chemical analyses performed on the bone emphasized the presence of arsenic, while the X-ray and CAT scan examinations revealed a quite big sella turcica. These two aspects might have influenced the performances of this athlete, and in the same time might have provoked his death at the age of about 30 years.

Ayudas ergogénicas en el deporte / Ergogenic aids in sport

Introducción: muy pocos suplementos nutricionales han demostrado científicamente su eficacia como ayuda ergogénica. Esta revisión analizará el monohidrato de creatina (MC), el β-hidroxi-β-metilbutirato (HMB), el bicarbonato sódico (BS), la β-alanina y la cafeína. Objetivos: analizar la eficacia, mecanismos de acción, dosis, efectos adversos y algunos deportes que se pueden beneficiar de su consumo. Métodos: búsqueda en la base de datos PubMed de revisiones bibliográficas de los últimos 15 años y artículos originales de los últimos 5 años de las sustancias estudiadas. Resultados: dosis de MC de 20 g/día durante 4-7 días son eficaces para mejorar la fuerza y la potencia muscular y el rendimiento en sprints cortos y repetidos. El HMB en dosis de 3 g/día durante un mínimo de 2 semanas contribuye al aumento de la masa magra y de la masa libre de grasa. La ingesta de 0,3 g/kg de BS mejora el rendimiento en pruebas de 400-1.500 m de atletismo y en sprints intermitentes. Por su parte, dosis de 80 mg/kg/día de β-alanina durante 4-10 semanas pueden mejorar el rendimiento en ejercicios intermitentes de alta intensidad. Finalmente, la cafeína en dosis de 2 mg/kg mejora la capacidad de reacción y en dosis de 3-6 mg/kg mejora el rendimiento en pruebas de resistencia aeróbica. Conclusiones: los suplementos revisados presentan una demostrada eficacia en el rendimiento físico, pero hay que tener en cuenta que la mayoría de los estudios se han realizado con deportistas de nivel recreativo. Generalmente, la mejora del rendimiento físico con estos suplementos es menor cuanto mejor es el nivel deportivo del individuo; sin embargo, un incremento de apenas un 1% permite a veces avanzar varios puestos en una final. Finalmente, se debe llamar la atención sobre la importancia de optimizar la alimentación antes de plantearse la introducción de suplementos deportivos, especialmente en niños y jóvenes. Las sustancias que hemos analizado poseen una base científica que respalda su efecto ergogénico. Todas ellas se pueden encontrar en el mercado con Certificado de Calidad y Pureza (AU)

Introduction: Very few nutritional supplements have scientifically demonstrated their effectiveness as an ergogenic aid. This review will examine creatine monohydrate (MC), the β-hydroxy-β-methylbutyrate (HMB), sodium bicarbonate (BS), the β-alanine and caffeine. Objectives: To analyze the efficacy, mechanisms of action, dose, side effects and some sports that can benefit from their consumption. Methods: Searching in PubMed bibliographic database reviews from the last 15 years and original articles from the last 5 years of the studied substances. Results: Doses of 20 mg/day for 4-7 days are effective in improving strength and muscular power and performance in short and repeated sprints. HMB at doses of 3 g/day for at least 2 weeks contributes to increased lean mass and fat-free mass. The intake of 0.3 g/kg of BS improves performance on tests of 400-1,500 meters in athletics and intermittent sprints. Meanwhile, doses of 80 mg/kg/day of β-alanine for 4-10 weeks may improve performance in high-intensity intermittent exercise. Finally, caffeine at doses of 2 mg/kg improves responsiveness and 3-6 mg/kg improves performance in endurance tests. Conclusions: The revised supplements have shown their efficacy in physical performance, but it is needed to keep in mind that most studies have been conducted with recreational-level athletes. Generally, the better the individual´s fitness level is the less improvement in physical performance the supplement shows. However, an increase of only 1% may sometimes allow the athlete to advance several positions in a final. Finally, we should draw attention to the importance of optimizing nutrition before considering the introduction of sports supplements, especially in children and youth. All analyzed substances have scientific basis supporting its ergogenic effect. All of them can be found in the market with Certificate of Quality and Purity (AU)

Efectos de la suplementación con testosterona sobre el rendimiento en resistencia / Efeitos da suplementação com testosterona sobre o desempenho da resistência / Effects of doping with testosterone on endurance performance

El dopaje en el deporte tiene su origen en la Grecia Clásica. Sin embargo, a lo largo del siglo pasado y hasta la actualidad, la utilización de este tipo de prácticas fraudulentas en el deporte ha ido en aumento. Entre las sustancias dopantes más utilizadas destacan la testosterona y sus derivados sintéticos, los anabolizantes sintéticos. A pesar de que estas sustancias prohibidas se han utilizado para la mejora del rendimiento en pruebas de fuerza y potencia, frecuentemente se detectan positivos en deportistas de resistencia. Los objetivos del presente estudio han sido informar acerca de los efectos ergogénicos de la suplementación con testosterona y anabolizantes sintéticos sobre el rendimiento en resistencia, a través de cambios sobre parámetros sanguíneos, así como los efectos secundarios que tienen sobre la salud. Para ello, se ha realizado una revisión en bases de datos como Elsevier, Medline, Pubmed y Web of Science incluyendo términos como testosterone, anemia, doping, endurance, erythropoietin, hepcidin e iron. La hepcidina se ha propuesto la principal reguladora de las reservas corporales de hierro y la suplementación con testosterona puede afectar a la síntesis de dicha hormona. Los efectos de la testosterona sobre la hepcidina podrían hacer mejorar tanto la capacidad de transporte como de difusión de oxígeno. De este modo, el dopaje con testosterona podría tener un potencial efecto ergogénico en modalidades de resistencia. Sin embargo, dichas mejoras pueden tener efectos negativos sobre el estado de salud del deportista, entre los que se encuentran trastornos metabólicos, orgánicos, psicológicos e inmunosupresión (AU)

Doping in sport has its origins in Ancient Greece. However, over the last century to the present, the use of such dishonest practices has increased. Among the most widely used performance enhancing drugs is the use of testosterone and its synthetics anabolics. Although these prohibited substances have been used to increase performance in test of strength and power, due to the ability to cause hypertrophy, very frequent it's detecting positive test doping by in endurance athletes by testosterone or synthetics anabolics. The aim of this study was to report the ergogenic effects of testosterone supplementation and synthetics anabolics on endurance performance, through changes on blood parameters. To this end, it has conducted a review in different databases such as Elsevier, Medline, Pubmed and Web of Science where terms such as testosterone, anemia, doping, endurance, erythropoietin, hepcidin and iron were included. Hepcidin has been proposed main regulator of body iron stores and testosterone supplementation may affect the synthesis of the hormone. The effects of testosterone on hepcidin could improve both transport capacity and oxygen diffusion. Thus, doping with testosterone could have a potential effect on ergogenic resistance patterns. However, such improvements can have negative effects on the health of the athlete like metabolic, organic, psychological disorders and immunosuppression (AU)

O doping no esporte tem suas origens na Grécia Antiga. No entanto, do último século para o presente, a utilização de tais práticas desonestas aumentou. Entre as drogas que melhoram o desempenho mais amplamente utilizadas são o uso de testosterona e seus anabolizantes sintéticos. Embora estas substâncias proibidas têm sido usados para aumentar o desempenho em testes de força e potência, devido à capacidade de causar hipertrofia, é muito frequentes detecção de doping por testosterona ou anabolizantes sintéticos no teste de atletas de endurance. O objetivo deste estudo foi relatar os efeitos ergogênicos da suplementação de testosterona e anabolizantes sintéticos sobre o desempenho de resistência, através de mudanças nos parâmetros sanguíneos. Para este efeito, procedeu a uma revisão em diferentes bancos de dados, tais como Elsevier, Medline, Pubmed e Web of Science, onde termos como a testosterona, anemia, doping, resistência, eritropoietina, hepcidina e ferro foram incluídos. Hepcidina foi proposto como principal regulador das reservas de ferro do corpo e a suplementação de testosterona pode afetar a síntese do hormonio. Os efeitos da testosterona sobre hepcidina poderia melhorar tanto a capacidade de transporte e difusão de oxigênio. Assim, a dopagem com testosterona pode ter um efeito potencial sobre padrões de resistência ergogênicos. No entanto, essas melhorias podem ter efeitos negativos sobre a saúde do atleta como metabolismo, distúrbios psicológicos orgânicos e imunossupressão (AU)

Emerging drugs affecting skeletal muscle function and mitochondrial biogenesis - Potential implications for sports drug testing programs.

RATIONALE: A plethora of compounds potentially leading to drug candidates that affect skeletal muscle function and, more specifically, mitochondrial biogenesis, has been under (pre)clinical investigation for rare as well as more common diseases. Some of these compounds could be the object of misuse by athletes aiming at artificial and/or illicit and drug-facilitated performance enhancement, necessitating preventive and proactive anti-doping measures. METHODS: Early warnings and the continuous retrieval and dissemination of information are crucial for sports drug testing laboratories as well as anti-doping authorities, as they assist in preparation of efficient doping control analytical strategies for potential future threats arising from new therapeutic developments. Scientific literature represents the main source of information, which yielded the herein discussed substances and therapeutic targets, which might become relevant for doping controls in the future. Where available, mass spectrometric data are presented, supporting the development of analytical strategies and characterization of compounds possibly identified in human sports drug testing samples. RESULTS & CONCLUSIONS: Focusing on skeletal muscle and mitochondrial biogenesis, numerous substances exhibiting agonistic or antagonistic actions on different cellular 'control centers' resulting in increased skeletal muscle mass, enhanced performance (as determined with laboratory animal models), and/or elevated amounts of mitochondria have been described. Substances of interest include agonists for REV-ERBα (e.g. SR9009, SR9011, SR10067, GSK4112), sirtuin 1 (e.g. SRT1720, SRT2104), adenosine monophosphate-activated protein kinase (AMPK, e.g. AICAR), peroxisome proliferator-activated receptor (PPAR)δ (e.g. GW1516, GW0742, L165041), and inhibitory/antagonistic agents targeting the methionine-folate cycle (MOTS-c), the general control non-derepressible 5 (GCN5) acetyl transferase (e.g. CPTH2, MB-3), myostatin (e.g. MYO-029), the myostatin receptor (bimagrumab), and myostatin receptor ligands (e.g. sotatercept, ACE-031). In addition, potentially relevant drug targets were identified, e.g. with the sarcoplasmic transmembrane peptide myoregulin and the nuclear receptor corepressor 1 (NCOR-1). The antagonism of these has shown to result in substantially enhanced physical performance in animals, necessitating the monitoring of strategies such as RNA interference regarding these substances. Most drug candidates are of lower molecular mass and comprise non-natural compositions, facts which suggest approaches for their qualitative identification in doping control samples by mass spectrometry. Electrospray ionization/collision-induced dissociation mass spectra of representatives of the aforementioned substances and selected in vitro derived phase-I metabolites support this assumption, and test methods for a subset of these have been recently established. Expanding the knowledge on analytical data will further facilitate the identification of such analytes and related compounds in confiscated material as well as sports drug testing specimens.

Performance-Enhancing Drugs I: Understanding the Basics of Testing for Banned Substances.

Whenever athletes willfully or accidentally ingest performance-enhancing drugs or other banned substances (such as drugs of abuse), markers of those drugs can be detected in biological samples (e.g., biofluids: urine, saliva, blood); in the case of some drugs, that evidence can be apparent for many weeks following the last exposure to the drug. In addition to the willful use of prohibited drugs, athletes can accidentally ingest banned substances in contaminated dietary supplements or foods and inadvertently fail a drug test that could mean the end of an athletic career and the loss of a good reputation. The proliferation of performance-enhancing drugs and methods has required a corresponding increase in the analytical tools and methods required to identify the presence of banned substances in biofluids. Even though extraordinary steps have been taken by organizations such as the World Anti-Doping Agency to limit the use of prohibited substances and methods by athletes willing to cheat, it is apparent that some athletes continue to avoid detection by using alternative doping regimens or taking advantage of the limitations in testing methodologies. This article reviews the testing standards and analytical techniques underlying the procedures used to identify banned substances in biological samples, setting the stage for future summaries of the testing required to establish the use of steroids, stimulants, diuretics, and other prohibited substances.

Practical experience with the implementation of an athlete's biological profile in athletics, cycling, football and swimming.

The introduction of the athlete's biological passport (ABP) has been a milestone in the fight against doping. The ABP is a collection of measurements of different biological parameters influenced by the administration of doping agents through the time and for each athlete. Two different modules have been developed and validated so far: the haematological module, which aims to identify enhancement of oxygen transport, including use of erythropoiesis-stimulating agents and any form of blood transfusion or manipulation, which became effective in 2010; and the steroidal module, which intends to detect the use of endogenous anabolic androgenic steroids when administered exogenously and other anabolic agents, which was introduced in 2014. Prior to the implementation of the haematological module, it is important to define an athlete's testing pool on whom to collect blood and/or urine in-competition and out-of-competition (for the steroidal module, this is irrelevant because all collected urine samples will be subjected to analysis for the steroidal variables) and to be compliant with the strict requirements of the World Anti-Doping Agency ABP Operating Guidelines. The established individual profile can be used either to target traditional antidoping tests (recombinant erythropoietins, or homologous blood transfusion tests for the haematological module; isotope ratio mass spectrometry (IRMS) for the steroidal module) or to support an antidoping rule violation due to the use of a forbidden substance or method. In this article, we present the experience of four major International Federations which have implemented an ABP programme, focusing on the haematological module. They constitute examples which could be followed by other antidoping organisations wishing to introduce this new, efficient and innovative antidoping tool.

LC-MS-MS analysis of dietary supplements for N-ethyl-α-ethyl-phenethylamine (ETH), N, N-diethylphenethylamine and phenethylamine.

There has been a recent rise in the number of cases of athletes being banned from competition because of positive tests for prohibited substances in their biological specimens. Most of these substances are on the World Anti-Doping Agency (WADA) prohibited list, while others are not specifically named on the list. N-Ethyl-α-ethyl-phenethylamine (ETH), a derivative of phenethylamine (PEA), is one of these unlisted substances and shares chemical and biological effects to the amphetamines, which are listed on the WADA prohibited substances list. It is classified as Category 6B stimulant on the list. This study was directed toward the development of an liquid chromatography tandem mass spectrometry (LC-MS-MS) method for the analysis of ETH in performance-enhancing dietary supplement. A standard was prepared and confirmed by spectroscopic analysis, which was then used to develop the analytical procedure. The procedure was validated and found to have an limit of detection of 2.5 ng/mL, limit of quantification of 5 ng/mL and upper limit of linearity of 500 ng/mL, with within-day variability at the 10-ng/mL level range of 3.88-7.89% (n = 6) and 1.39-3.36% (n = 6) for the 100-ng/mL level. The day-to-day variability was 9.8% for the low control and 3.1% for the high control. The method was used to analyze a variety of dietary supplements for ETH as well as PEA and its N, N-diethyl derivative (NDP).

No improvement in endurance performance after a single dose of beetroot juice.

INTRODUCTION: Dietary nitrate supplementation has received much attention in the literature due to its proposed ergogenic properties. Recently, the ingestion of a single bolus of nitrate-rich beetroot juice (500 ml, ~6.2 mmol NO3-) was reported to improve subsequent time-trial performance. However, this large volume of ingested beetroot juice does not represent a realistic dietary strategy for athletes to follow in a practical, performance-based setting. Therefore, we investigated the impact of ingesting a single bolus of concentrated nitrate-rich beetroot juice (140 ml, ~8.7 mmol NO3-) on subsequent 1-hr time-trial performance in well-trained cyclists. METHODS: Using a double-blind, repeated-measures crossover design (1-wk washout period), 20 trained male cyclists (26 ± 1 yr, VO(2peak) 60 ± 1 ml · kg(-1) · min(-1), Wmax 398 ± 7.7 W) ingested 140 ml of concentrated beetroot juice (8.7 mmol NO3-; BEET) or a placebo (nitrate-depleted beetroot juice; PLAC) with breakfast 2.5 hr before an ~1-hr cycling time trial (1,073 ± 21 kJ). Resting blood samples were collected every 30 min after BEET or PLAC ingestion and immediately after the time trial. RESULTS: Plasma nitrite concentration was higher in BEET than PLAC before the onset of the time trial (532 ± 32 vs. 271 ± 13 nM, respectively; p < .001), but subsequent time-trial performance (65.5 ± 1.1 vs. 65 ± 1.1 s), power output (275 ± 7 vs. 278 ± 7 W), and heart rate (170 ± 2 vs. 170 ± 2 beats/min) did not differ between BEET and PLAC treatments (all p > .05). CONCLUSION: Ingestion of a single bolus of concentrated (140 ml) beetroot juice (8.7 mmol NO3-) does not improve subsequent 1-hr time-trial performance in well-trained cyclists.

1,3-Dimethylamylamine (DMAA) in supplements and geranium products: natural or synthetic?

1,3-Dimethylamylamine (DMAA) is a stimulant existing in various pre-workout supplements and often labelled as part of geranium plants. The safety and origin of DMAA in these supplements is the subject of intense debate. In this study, the enantiomeric and diastereomeric ratios of two different known synthetic DMAA compounds, as well as the total concentrations of DMAA and its stereoisomeric ratios in 13 different supplements, were determined by gas chromatography. The stereoisomeric ratios of DMAA in the synthetic standards and in all the commercial supplements were indistinguishable. Eight different commercial geranium extracts of different geographical origins (China and the Middle East) were examined for the presence of DMAA by high performance liquid chromatography coupled with mass spectrometry (HPLC-MS). No DMAA was detected in any of the eight geranium products with a limit of detection of 10 parts per billion (w/w).

Whole beetroot consumption acutely improves running performance.

Nitrate ingestion improves exercise performance; however, it has also been linked to adverse health effects, except when consumed in the form of vegetables. The purpose of this study was to determine, in a double-blind crossover study, whether whole beetroot consumption, as a means for increasing nitrate intake, improves endurance exercise performance. Eleven recreationally fit men and women were studied in a double-blind placebo controlled crossover trial performed in 2010. Participants underwent two 5-km treadmill time trials in random sequence, once 75 minutes after consuming baked beetroot (200 g with ≥500 mg nitrate) and once 75 minutes after consuming cranberry relish as a eucaloric placebo. Based on paired t tests, mean running velocity during the 5-km run tended to be faster after beetroot consumption (12.3±2.7 vs 11.9±2.6 km/hour; P=0.06). During the last 1.1 miles (1.8 km) of the 5-km run, running velocity was 5% faster (12.7±3.0 vs 12.1±2.8 km/hour; P=0.02) in the beetroot trial, with no differences in velocity (P≥0.25) in the earlier portions of the 5-km run. No differences in exercise heart rate were observed between trials; however, at 1.8 km into the 5-km run, rating of perceived exertion was lower with beetroot (13.0±2.1 vs 13.7±1.9; P=0.04). Consumption of nitrate-rich, whole beetroot improves running performance in healthy adults. Because whole vegetables have been shown to have health benefits, whereas nitrates from other sources may have detrimental health effects, it would be prudent for individuals seeking performance benefits to obtain nitrates from whole vegetables, such as beetroot.